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Buy Ketamine Crystals near me.A medication used for anesthesia to stop pain during surgeries.
DrugBank IDDB01221
TypeSmall Molecule
US ApprovedYES
Other ApprovedYES
Clinical Trials

Phase 0

52
Phase 1

149
Phase 2

285
Phase 3

196
Phase 4

380
Therapeutic Categories

  • Anesthetics, General 

Identification

Summary
Ketamine is a rapid-acting general anesthetic and NMDA receptor antagonist used for induction of anesthesia diagnostic and surgical procedures typically in combination with a muscle relaxant.Buy Ketamine Crystals near me
Brand Names
Ketalar
Generic Name
Ketamine
DrugBank Accession Number
DB01221
Background
Ketamine is an NMDA receptor antagonist with a potent anesthetic effect.6 It was developed in 1963 as a replacement for phencyclidine (PCP) by Calvin Stevens at Parke Davis Laboratories. It started being used for veterinary purposes in Belgium and in 1964 was proven that compared to PCP, it produced minor hallucinogenic effects and shorter psychotomimetic effects. It was FDA approved in 1970, and from there, it has been used as an anesthetic for children or patients undergoing minor surgeries but mainly for veterinary purposes.14
Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Structure
Weight
Average: 237.725
Monoisotopic: 237.092041846
Chemical Formula
C13H16ClNO
Synonyms
  • DL-ketamine
  • Ketamina
  • Kétamine
  • Ketamine
  • Ketaminum
  • NMDA
External IDs

  • 100477-72-3
  • NSC-70151

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Pharmacology

Indication
Ketamine is indicated as an anesthetic agent for recommended diagnostic and surgical procedures. If skeletal muscle relaxation is needed, it should be combined with a muscle relaxant. If the surgical procedure involves visceral pain, it should be supplemented with an agent that obtunds visceral pain. Ketamine can be used for induction of anesthesia prior other general anesthetic agents and as a supplement of low potency agents.15,LabelReports have indicated a potential use of ketamine as a therapeutic tool for the management of depression when administered in lower doses.7 These reports have increased the interest for ketamine in this area and several clinical trials are launched for this indication.16,8

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Associated Therapies

Contraindications & Blackbox Warnings

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Pharmacodynamics
Ketamine is a rapid-acting general anesthetic producing an anesthetic state characterized by profound analgesia, normal pharyngeal-laryngeal reflexes, normal or slightly enhanced skeletal muscle tone, cardiovascular and respiratory stimulation, and occasionally a transient and minimal respiratory depression. The anesthetic state produced by Ketamine has been termed as “dissociative anesthesia” in that it appears to selectively interrupt association pathways of the brain before producing somesthetic sensory blockade. It may selectively depress the thalamoneocortical system before significantly obtunding the more ancient cerebral centers and pathways (reticular-activating and limbic systems).2Ketamine enhances descending inhibiting serotoninergic pathways and can exert antidepressive effects. These effects are seen in concentrations ten times lower than the needed concentration for anesthetic proposes. The effect of ketamine can be described as analgesic by the prevention of central sensitization in dorsal horn neurons as well as by the inhibition on the synthesis of nitric oxide. Ketamine can present cardiovascular changes and bronchodilatation.9
Mechanism of action
Ketamine interacts with N-methyl-D-aspartate (NMDA) receptors, opioid receptors, monoaminergic receptors, muscarinic receptors and voltage sensitive Ca ion channels. Unlike other general anaesthetic agents, ketamine does not interact with GABA receptors.5

Target Actions Organism
AGlutamate receptor ionotropic, NMDA 3A
antagonist
Humans
A5-hydroxytryptamine receptor 3A
potentiator
Humans
ANeuronal acetylcholine receptor subunit alpha-7
antagonist
Humans
ACholinesterase
inhibitor
Humans
ANitric oxide synthase 1
inhibitor
Humans
USubstance-P receptor
antagonist
Humans
UD(2) dopamine receptor
agonist
partial agonist
Humans
UDelta-type opioid receptor
binder
Humans
USodium-dependent noradrenaline transporter
inhibitor
Humans
UKappa-type opioid receptor
agonist
Humans
UMu-type opioid receptor
binder
Humans
UMuscarinic acetylcholine receptor
binder
Humans
U5-hydroxytryptamine receptor 2
antagonist
Humans
U5-hydroxytryptamine receptor 1
antagonist
Humans
Absorption
Ketamine absorption is very rapid and the bioavailability is around 93%. After the first pass metabolism, only 17% of the administered dose is absorbed.10 It distributes very rapidly and presents a distribution half-life of 1.95 min.12 The Cmax levels at peak reach 0.75 mcg/ml in plasma and 0.2 mcg/ml in cerebrospinal fluid.15
Volume of distribution
The apparent volume of distribution of the central compartment and at steady-state are 371.3 ml/kg and 4060.3 ml/kg, respectively.13
Protein binding
The plasma protein binding of ketamine accounts for 53.5% of the administered dose.12
Metabolism
Ketamine presents a mainly hepatic metabolism and its major metabolite is norketamine. The biotransformation of ketamine corresponds to N-dealkylation, hydroxylation of the cyclohexone ring, conjugation to glucuronic acid and dehydration of the hydroxylated metabolites for the formation of cyclohexene derivatives.10

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Route of elimination
Pharmacokinetic studies have resulted in the recovery of 85-95% of the administered dose in urine mainly in the form of metabolites. Some other routes of elimination of ketamine are bile and feces. When administered intravenously the resultant recovery is distributed by 91% of the administered dose in urine and 3% in feces.15
Half-life
The reported half-life in preclinical studies for ketamine is 186 min.10
Clearance
The clearance rate of ketamine is high and of around 95 L/h/70kg.11
Adverse Effects

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Toxicity
Preclinical studies related to the blocking of NMDA receptors have shown an increase in apoptosis in the developing brain which results in cognitive deficits when used for longer than 3 hours. Toxicity studies regarding carcinogenesis have not been performed. Regarding mutagenesis and fertility, ketamine showed to be clastogenic and to not have effects on fertility.Label
Pathways
Not Available
Pharmacogenomic Effects/ADRs

Not Available

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Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Buy ketamine – ketamine for sale – liquid ketamine for sale
Food Interactions
  • Avoid alcohol.

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Product Ingredients

Ingredient UNII CAS InChI Key
Ketamine hydrochloride O18YUO0I83 1867-66-9 VCMGMSHEPQENPE-UHFFFAOYSA-N
International/Other Brands
Ketaject (Bristol-Myers Squibb) / Ketanest (Parke Davis)
Brand Name Prescription Products
Generic Prescription Products
Unapproved/Other Products

Categories

ATC Codes
N01AX03 — Ketamine

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as chlorobenzenes. These are compounds containing one or more chlorine atoms attached to a benzene moiety.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Halobenzenes
Direct Parent
Chlorobenzenes
Alternative Parents
Aralkylamines / Aryl chlorides / Cyclic ketones / Dialkylamines / Organopnictogen compounds / Organochlorides / Organic oxides / Hydrocarbon derivatives
Substituents
Amine / Aralkylamine / Aromatic homomonocyclic compound / Aryl chloride / Aryl halide / Carbonyl group / Chlorobenzene / Cyclic ketone / Hydrocarbon derivative / Ketone
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
secondary amino compound, monochlorobenzenes, cyclohexanones (CHEBI:6121)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
690G0D6V8H
CAS number
6740-88-1
InChI Key
YQEZLKZALYSWHR-UHFFFAOYSA-N
InChI
InChI=1S/C13H16ClNO/c1-15-13(9-5-4-8-12(13)16)10-6-2-3-7-11(10)14/h2-3,6-7,15H,4-5,8-9H2,1H3
IUPAC Name
2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one
SMILES
CNC1(CCCCC1=O)C1=CC=CC=C1Cl

References

Synthesis Reference
John A. Flores, Kenton L. Crowley, “Process for the preparation of ketamine ointment.” U.S. Patent US5817699, issued June, 1995.US5817699
General References
  1. Harrison NL, Simmonds MA: Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral cortex. Br J Pharmacol. 1985 Feb;84(2):381-91. [Article]
  2. Bergman SA: Ketamine: review of its pharmacology and its use in pediatric anesthesia. Anesth Prog. 1999 Winter;46(1):10-20. [Article]
  3. Bonanno FG: Ketamine in war/tropical surgery (a final tribute to the racemic mixture). Injury. 2002 May;33(4):323-7. [Article]
  4. Lankenau SE, Sanders B, Bloom JJ, Hathazi D, Alarcon E, Tortu S, Clatts MC: First injection of ketamine among young injection drug users (IDUs) in three U.S. cities. Drug Alcohol Depend. 2007 Mar 16;87(2-3):183-93. Epub 2006 Sep 18. [Article]
  5. Reboso Morales JA, Gonzalez Miranda F: [Ketamine]. Rev Esp Anestesiol Reanim. 1999 Mar;46(3):111-22. [Article]
  6. Ivani G, Vercellino C, Tonetti F: Ketamine: a new look to an old drug. Minerva Anestesiol. 2003 May;69(5):468-71. [Article]
  7. Yang Y, Cui Y, Sang K, Dong Y, Ni Z, Ma S, Hu H: Ketamine blocks bursting in the lateral habenula to rapidly relieve depression. Nature. 2018 Feb 14;554(7692):317-322. doi: 10.1038/nature25509. [Article]
  8. Kirby T: Ketamine for depression: the highs and lows. Lancet Psychiatry. 2015 Sep;2(9):783-4. doi: 10.1016/S2215-0366(15)00392-2. [Article]
  9. Xu J, Lei H: Ketamine-an update on its clinical uses and abuses. CNS Neurosci Ther. 2014 Dec;20(12):1015-20. doi: 10.1111/cns.12363. [Article]
  10. Clements JA, Nimmo WS, Grant IS: Bioavailability, pharmacokinetics, and analgesic activity of ketamine in humans. J Pharm Sci. 1982 May;71(5):539-42. [Article]
  11. Fanta S, Kinnunen M, Backman JT, Kalso E: Population pharmacokinetics of S-ketamine and norketamine in healthy volunteers after intravenous and oral dosing. Eur J Clin Pharmacol. 2015 Apr;71(4):441-7. doi: 10.1007/s00228-015-1826-y. Epub 2015 Mar 1. [Article]
  12. Kaka JS, Hayton WL: Pharmacokinetics of ketamine and two metabolites in the dog. J Pharmacokinet Biopharm. 1980 Apr;8(2):193-202. [Article]
  13. Pypendop BH, Ilkiw JE: Pharmacokinetics of ketamine and its metabolite, norketamine, after intravenous administration of a bolus of ketamine to isoflurane-anesthetized dogs. Am J Vet Res. 2005 Dec;66(12):2034-8. doi: 10.2460/ajvr.2005.66.2034. [Article]
  14. Ketamine [Link]
  15. Ketamine monograph [Link]
  16. Time magazine [Link]
Human Metabolome Database
HMDB0015352
KEGG Drug
D08098
KEGG Compound
C07525
PubChem Compound
3821
PubChem Substance
46508295
ChemSpider
3689
BindingDB
50044140
RxNav
6130
ChEBI
6121
ChEMBL
CHEMBL742
Therapeutic Targets Database
DAP001148
PharmGKB
PA450144
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ketamine
FDA label
Download (228 KB)
MSDS
Download (67.5 KB)

Clinical Trials

Clinical Trials

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Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Bioniche Pharma
  • Hospira Inc.
  • JHP Pharmaceuticals LLC
  • Medisca Inc.
  • Monarch Pharmacy
  • Pharmedium
  • Physicians Total Care Inc.
Dosage Forms
Prices
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
Property Value Source
melting point (°C) 92.5ºC Medical toxicology of drug abuse. (2012)
water solubility Soluble ‘MSDS’
logP 3.120 Medical toxicology of drug abuse. (2012)
pKa 7.5 Ketamine monograph
Predicted Properties
Property Value Source
Water Solubility 0.0464 mg/mL ALOGPS
logP 2.69 ALOGPS
logP 3.35 Chemaxon
logS -3.7 ALOGPS
pKa (Strongest Acidic) 19.77 Chemaxon
pKa (Strongest Basic) 7.16 Chemaxon
Physiological Charge 1 Chemaxon
Hydrogen Acceptor Count 2 Chemaxon
Hydrogen Donor Count 1 Chemaxon
Polar Surface Area 29.1 Å2 Chemaxon
Rotatable Bond Count 2 Chemaxon
Refractivity 65.55 m3·mol-1 Chemaxon
Polarizability 24.97 Å3 Chemaxon
Number of Rings 2 Chemaxon
Bioavailability 1 Chemaxon
Rule of Five Yes Chemaxon
Ghose Filter Yes Chemaxon
Veber’s Rule Yes Chemaxon
MDDR-like Rule No Chemaxon
Predicted ADMET Features
Property Value Probability
Human Intestinal Absorption + 0.9974
Blood Brain Barrier + 0.9826
Caco-2 permeable + 0.6326
P-glycoprotein substrate Substrate 0.5753
P-glycoprotein inhibitor I Non-inhibitor 0.5948
P-glycoprotein inhibitor II Non-inhibitor 0.8383
Renal organic cation transporter Non-inhibitor 0.6737
CYP450 2C9 substrate Non-substrate 0.6363
CYP450 2D6 substrate Substrate 0.8918
CYP450 3A4 substrate Substrate 0.7407
CYP450 1A2 substrate Non-inhibitor 0.7323
CYP450 2C9 inhibitor Non-inhibitor 0.7985
CYP450 2D6 inhibitor Non-inhibitor 0.6912
CYP450 2C19 inhibitor Non-inhibitor 0.5347
CYP450 3A4 inhibitor Non-inhibitor 0.8253
CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.5426
Ames test Non AMES toxic 0.7223
Carcinogenicity Non-carcinogens 0.8878
Biodegradation Not ready biodegradable 0.9937
Rat acute toxicity 2.3939 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.8859
hERG inhibition (predictor II) Inhibitor 0.6047
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum – GC-MS Predicted GC-MS splash10-0ue9-1900000000-137b9855ffed670aa9f4
LC-MS/MS Spectrum – LC-ESI-QTOF , positive LC-MS/MS splash10-004i-0930000000-8216e02922628a5070cf
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-00di-0090000000-7704dbbfa717abc4bab2
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-000i-0090000000-aff2b684d97275321043
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-000i-0290000000-1707dec51cc3e89964c9
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-004i-0940000000-59871faec16835eb1b3a
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-004i-0900000000-ca62e82b4a1dfb81b3b0
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-004i-0900000000-6c243d7b1c2e8cf69efa
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-004i-0900000000-441a423105753e2c8b9c
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-000i-0090000000-24585e7c2431b3b9319e
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-000i-0290000000-c9d734b085ec94dabd9a
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-004i-0940000000-054d77385726d4e35e20
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-004i-0900000000-8c263bb521fb6ebe6cac
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-004i-0900000000-702873d66ce0d419711d
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-004i-0900000000-e23ba411aa96df9b5d6f
LC-MS/MS Spectrum – LC-ESI-ITFT , positive LC-MS/MS splash10-00di-0090000000-5f14196db213c95f3e71
LC-MS/MS Spectrum – LC-ESI-QQ , positive LC-MS/MS splash10-000i-0090000000-85385cf96aa2ac05921a
LC-MS/MS Spectrum – LC-ESI-QQ , positive LC-MS/MS splash10-05br-0390000000-9177663a5915fac51aa7
LC-MS/MS Spectrum – LC-ESI-QQ , positive LC-MS/MS splash10-004i-0910000000-d00d242dae695dc5aff9
LC-MS/MS Spectrum – LC-ESI-QQ , positive LC-MS/MS splash10-004i-0900000000-95c2a8805f1587266fea
LC-MS/MS Spectrum – LC-ESI-QQ , positive LC-MS/MS splash10-004i-1900000000-9e61adc80771178de9d3
LC-MS/MS Spectrum – LC-ESI-IT , positive LC-MS/MS splash10-00di-0190000000-686c139c454aea662d84
Predicted MS/MS Spectrum – 10V, Positive (Annotated) Predicted LC-MS/MS splash10-000i-0980000000-bded2bdf9853c6184bf1
Predicted MS/MS Spectrum – 10V, Negative (Annotated) Predicted LC-MS/MS splash10-000i-0090000000-f329d25c0537015062fc
Predicted MS/MS Spectrum – 20V, Positive (Annotated) Predicted LC-MS/MS splash10-052u-0890000000-7934d3aa418dfbf17488
Predicted MS/MS Spectrum – 20V, Negative (Annotated) Predicted LC-MS/MS splash10-052r-2290000000-f29c223b2da48a50baf6
Predicted MS/MS Spectrum – 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0avr-1910000000-c2a25e54634de389a8a5
Predicted MS/MS Spectrum – 40V, Negative (Annotated) Predicted LC-MS/MS splash10-000w-9110000000-3c59d084c31e14c73fad
Predicted 1H NMR Spectrum 1D NMR Not Applicable
Predicted 13C NMR Spectrum 1D NMR Not Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source
[M-H]- 152.3173949
predicted
DarkChem Lite v0.1.0
[M-H]- 149.78523
predicted
DeepCCS 1.0 (2019)
[M+H]+ 152.3352949
predicted
DarkChem Lite v0.1.0
[M+H]+ 152.14323
predicted
DeepCCS 1.0 (2019)
[M+Na]+ 152.3356949
predicted
DarkChem Lite v0.1.0
[M+Na]+ 159.28464
predicted
DeepCCS 1.0 (2019)

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